A simple synthesis of APM ([p-(N-acrylamino)-phenyl]mercuric chloride), a useful tool for the analysis of thiolated biomolecules.

abstract：:A series of 2-phenylpyrimidine coumarin derivatives with potential telomerase-inhibiting activity was designed and synthesized. All of the compounds were screened for antiproliferative activity against CNE2, KB, and Cal27 cell lines in vitro. The results showed that most of the derivatives had a favorable effect on re...

journal_title：Bioorganic & medicinal chemistry letters

authors： Lv N,Sun M,Liu C,Li J

更新日期：2017-10-01 00:00:00

abstract：:A single-step sensing system was developed to visually detect ligands of a cleavase-like RNA aptazyme at room temperature using aptazyme-tethered gold nanoparticles, the electrosteric stability of which was adjusted by increasing their diameter. In this system, the ligand induces self-cleavage of the aptazyme on gold ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ogawa A

更新日期：2011-01-01 00:00:00

abstract：:To improve the drug-ability of celastrol, a series of PEGylation celastrol (PEGC) were designed and synthesized by conjugation with different kinds of polyethylene glycols (PEGs) with celastrol. Most of PEGCs could easily dissolve in water. In particular, one of them (DC1000) could be dispersed in water to form nanopa...

journal_title：Bioorganic & medicinal chemistry letters

authors： Shan WG,Wang HG,Wu R,Zhan ZJ,Ma LF

更新日期：2019-03-01 00:00:00

abstract：:Starting from thienobenzopyran HTS hit 1, co-crystallization, molecular modeling and metabolic analysis were used to design potent and metabolically stable inhibitors of PI3-kinase. Compound 15 demonstrated PI3K pathway suppression in a mouse MCF7 xenograft model. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Staben ST,Siu M,Goldsmith R,Olivero AG,Do S,Burdick DJ,Heffron TP,Dotson J,Sutherlin DP,Zhu BY,Tsui V,Le H,Lee L,Lesnick J,Lewis C,Murray JM,Nonomiya J,Pang J,Prior WW,Salphati L,Rouge L,Sampath D,Sideris S,

更新日期：2011-07-01 00:00:00

abstract：:Relying on the high affinities of the benz-indolo-azecine LE 300 (1) and the hydroxylated dibenz-azecine LE 404 (2b) for the D1/D5 receptor subtypes, we synthesized methoxylated, hydroxylated and an indole-N methylated derivatives of 1 (Fig. 1). Hydroxylation of azecine derivatives is beneficial with regard to the aff...

journal_title：Bioorganic & medicinal chemistry letters

authors： Enzensperger C,Kilian S,Ackermann M,Koch A,Kelch K,Lehmann J

更新日期：2007-03-01 00:00:00

abstract：:The DBU-promoted intramolecular aldol condensation of two partially protected L-lyxo-hexos-5-ulose derivatives (8 and 9), in turn obtained starting from methyl beta-D-galactopyranoside, takes place with fairly good yield and complete diastereoselectivity to give 2L-(2,3,6/4,5)-pentahydroxycyclohexanone derivatives, 10...

journal_title：Bioorganic & medicinal chemistry letters

authors： Catelani G,Corsaro A,D'Andrea F,Mariani M,Pistarà V

更新日期：2002-11-18 00:00:00

abstract：:The 1,2,3-triazole ring fused with pyridine/pyrimidine was explored as new template for the identification of potential antimicrobial agents. The regioselective synthesis of these pre-designed N-heteroarenes was achieved via exploring the application of Buchwald's strategy (i.e. C-N bond formation/reduction/diazotizat...

journal_title：Bioorganic & medicinal chemistry letters

authors： Marepu N,Yeturu S,Pal M

更新日期：2018-11-01 00:00:00

abstract：:A novel type of caspase inhibitor prodrug that improves systemic exposure after oral administration in rats has been designed. Such a prodrug, based on a 6,6a-dihydrofuro[3,2-d]oxazol-5(3aH)-one motif, has the advantage of rapidly liberating the active inhibitor without producing any cleavage by-product. Prodrugs 6-8,...

journal_title：Bioorganic & medicinal chemistry letters

authors： Charrier JD,Durrant SJ,Studley J,Lawes L,Weber P

更新日期：2012-01-01 00:00:00

abstract：:The radical-scavenging capacities of ferrocenyl group and phenolic hydroxyl group in ferrocenyl chalcone were identified in this work. 1,1'-Diacetylferrocene was applied to condense with benzaldehyde, vanillin, and protocatechualdehyde to produce ferrocenyl chalcones, which were employed to interact with 2,2'-azinobis...

journal_title：Bioorganic & medicinal chemistry letters

authors： Nabi G,Liu ZQ

更新日期：2011-02-01 00:00:00

abstract：:A series of indole ring containing compounds were designed based on the structure of the gp41 complex in the region of the hydrophobic pocket. These compounds were synthesized using a Suzuki Coupling reaction, and evaluated using a fluorescence binding assay and cell-cell fusion assay. The observed inhibition constant...

journal_title：Bioorganic & medicinal chemistry letters

authors： Zhou G,Wu D,Hermel E,Balogh E,Gochin M

更新日期：2010-03-01 00:00:00

abstract：:A new class of inhibitors of HIV-1 integrase has been optimized to provide selective and highly efficient strand transfer inhibition. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Donghi M,Kinzel OD,Summa V

更新日期：2009-04-01 00:00:00

abstract：:A series of pentapeptides, based on hMC4R pentapeptide agonist (Bu-His(6)-DPhe(7)-Arg(8)-Trp(9)-Gly(10)-NH(2)), was prepared in which either DPhe(7) or Trp(9) residue was systematically substituted. A number of interesting DPhe surrogates (D-Thi, D-3-CF(3)Phe, D-2-Nal and D-3,4-diClPhe) as well as Trp surrogates (2-Na...

journal_title：Bioorganic & medicinal chemistry letters

authors： Danho W,Swistok J,Cheung AW,Kurylko G,Franco L,Chu XJ,Chen L,Yagaloff K

更新日期：2003-02-24 00:00:00

abstract：:The seminal human dopamine D3 receptor (hD3R) ligand BP 897 has shown interesting properties during clinical trials. However, its lack of selectivity towards human adrenergic receptor impedes further development. Two approaches were followed to increase hD3R selectivity. The lead optimisation succeeded, we disclose he...

journal_title：Bioorganic & medicinal chemistry letters

authors： Capet M,Calmels T,Levoin N,Danvy D,Berrebi-Bertrand I,Stark H,Schwartz JC,Lecomte JM

更新日期：2016-02-01 00:00:00

abstract：:A novel class of indomethacin analogs were synthesized wherein a N-difluoromethyl-1,2-dihydropyrid-2-one moiety (5-LOX pharmacophore) was attached at its C-4 or C-5 position via either a CO (14a-b) or CH(2) (19a-b) linker to the indole N(1)-position. In this regard, replacement of the 4-chlorobenzoyl group present in ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Chowdhury MA,Huang Z,Abdellatif KR,Dong Y,Yu G,Velázquez CA,Knaus EE

更新日期：2010-10-01 00:00:00

abstract：:We designed and synthesized strobilurin analogues as hypoxia-inducible factor (HIF) inhibitors based on the molecular structure of kresoxim-methyl. Biological evaluation in human colorectal cancer HCT116 cells showed that most of the synthesized kresoxim-methyl analogues possessed moderate to potent inhibitory activit...

journal_title：Bioorganic & medicinal chemistry letters

authors： Lee S,Kwon OS,Lee CS,Won M,Ban HS,Ra CS

更新日期：2017-07-01 00:00:00

abstract：:This Letter describes, for the first time, the synthesis and SAR, developed through an iterative analog library approach, that led to the discovery of the positive allosteric modulator (PAM) of the metabotropic glutamate receptor mGluR5 CPPHA. Binding to a unique allosteric binding site distinct from other mGluR5 PAMs...

journal_title：Bioorganic & medicinal chemistry letters

authors： Zhao Z,Wisnoski DD,O'Brien JA,Lemaire W,Williams DL Jr,Jacobson MA,Wittman M,Ha SN,Schaffhauser H,Sur C,Pettibone DJ,Duggan ME,Conn PJ,Hartman GD,Lindsley CW

更新日期：2007-03-01 00:00:00

abstract：:Systematic SAR studies of the different regioisomers and homologues of the spiro(indane-1,4-piperidine) moiety in the growth hormone secretagogue L-162,752 are presented. Among them, spiro(3H-1-benzopyran-2,3-piperidine) was found to afford secretagogues with low nanomolar in vitro activity. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Yang L,Morriello G,Prendergast K,Cheng K,Jacks T,Chan WW,Schleim KD,Smith RG,Patchett AA

更新日期：1998-01-06 00:00:00

abstract：:P21-activated kinase 1 (PAK1) plays a vital role in the proliferation, survival and migration of cancer cells, which has emerged as a promising drug target for cancer therapy. In this study, a series of 2-indolinone derivatives were designed and synthesized through a structure-based strategy. A potent PAK1 inhibitor (...

journal_title：Bioorganic & medicinal chemistry letters

authors： Yao D,Ruhan A,Jiang J,Huang J,Wang J,Han W

更新日期：2020-09-01 00:00:00

abstract：:4-Thiazolidinone derivatives were synthesized using T3P®-DMSO media as a cyclodehydrating agent. All the molecules were tested for their cytotoxicity against leukemic cell lines. The compound 3-(4-bromophenyl)-2-(4-(dimethylamino)phenyl)thiazolidin-4-one (4e) with electron donating substituent at para position of phen...

journal_title：Bioorganic & medicinal chemistry letters

authors： Sharath Kumar KS,Hanumappa A,Vetrivel M,Hegde M,Girish YR,Byregowda TR,Rao S,Raghavan SC,Rangappa KS

更新日期：2015-09-01 00:00:00

abstract：:Macrocarpins A (1), B (2), C (3) and D (4), four new nor-triterpenes, have been isolated from the roots of Maytenus macrocarpa. The structures were established by spectroscopic examinations. Natural compounds 1, 2, 4 and the acetyl derivative 1a are cytotoxic against four tumoral cell lines with IC50 values ranging be...

journal_title：Bioorganic & medicinal chemistry letters

authors： Chávez H,Rodríguez G,Estévez-Braun A,Ravelo AG,Estévez-Reyes R,González AG,Fdez-Puente JL,García-Grávalos D

更新日期：2000-04-17 00:00:00

abstract：:(Me)FGC(Bz)DEVD was radiolabeled with technetium-99m in high yield. This tracer was preferentially accumulated in apoptotic cells in the in vitro studies. Tumor uptake occurred in vivo after cisplatin injection due to the apoptosis induction, which not observed in the untreated tumors. Therefore, (99m)Tc-(Me)FGCDEVD i...

journal_title：Bioorganic & medicinal chemistry letters

authors： Bohn P,Mouchard F,Rouvet J,de Boisgrollier AC,Vera P

更新日期：2013-03-01 00:00:00

abstract：:We have designed, synthesized, and evaluated the factor Xa inhibitory activities of p-amidinophenyl-sulfones, amines, and alcohols intended to take advantage of the polarity and hydrogen-bonding potential of the oxyanion hole region of the S1 specificity pocket. We demonstrate that placement of an anionic group within...

journal_title：Bioorganic & medicinal chemistry letters

authors： Rumthao S,Lee O,Sheng Q,Fu W,Mulhearn DC,Crich D,Mesecar AD,Johnson ME

更新日期：2004-10-18 00:00:00

abstract：:Arenobufagin is a naturally occurring bufadienolide showing promising antitumor activity accompanied however with apparent cardiac toxicity. Following the recent discovery that oxidative damage possibly be an important cause of the cardiac toxicity of cardenolides, a strategy fusing the antitumor agent arenobufagin wi...

journal_title：Bioorganic & medicinal chemistry letters

authors： Hou W,Huang ZX,Xu HG,Lin J,Zhang DM,Peng QL,Lin H,Chang YQ,Wang LH,Yao Z,Sun PH,Chen WM

更新日期：2018-11-01 00:00:00

abstract：:Constraining the catechol aryl ether moiety of bastadins by incorporation into a macrocyle is not necessary in order to mimic the effects of these marine natural products on neuronal calcium homeostasis. Simple, acyclic analogs that embody the 'western' or 'eastern' parts of bastadins were found to evoke comparable re...

journal_title：Bioorganic & medicinal chemistry letters

authors： Zieminska E,Lazarewicz JW,Couladouros EA,Moutsos VI,Pitsinos EN

更新日期：2008-11-01 00:00:00

abstract：:Clausenamide, isolated from aqueous extract of dry leaves of Clausena lansium, a Chinese folk medicine, was found to have potent activity in enhancing LTP and show nootropic activity in animal tests. In order to discovery more potent stereoisomers and to analyze the relationship of structure-activity, the synthesis of...

journal_title：Bioorganic & medicinal chemistry letters

authors： Feng Z,Li X,Zheng G,Huang L

更新日期：2009-04-15 00:00:00

abstract：:In order to obtain rigidity within the sugar moiety of nucleosides, the bicyclic pyrimidine derivatives of N,O-isoxazolidines were designed and synthesized by using 1,3-dipolar cycloaddition of Delta(1)-pyrrolidine-1-oxide and the appropriate vinyl-nucleobases. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Procopio A,Alcaro S,De Nino A,Maiuolo L,Ortuso F,Sindona G

更新日期：2005-02-01 00:00:00

abstract：:The novel analysis method consisting of size-exclusion chromatography (SEC) and HRMS analysis was firstly applied in the discovery of potential inhibitors towards cancer drug targets. With vascular endothelial growth factor receptor (VEGFR-2) as a target, dynamic combinatorial libraries (DCLs) were prepared by reactin...

journal_title：Bioorganic & medicinal chemistry letters

authors： Yang Z,Fang Z,He W,Wang Z,Gan H,Tian Q,Guo K

更新日期：2016-04-01 00:00:00

abstract：:A series of COX-2 selective inhibitor nimesulide derivatives were synthesized. Their anti-cell proliferation activities were evaluated with a long-term estrogen deprived MCF-7aro (LTEDaro) breast cancer cell line, which is the biological model of aromatase inhibitor resistance for hormone-dependent breast cancer. Comp...

journal_title：Bioorganic & medicinal chemistry letters

authors： Su B,Chen S

更新日期：2009-12-01 00:00:00

abstract：:Considering the complex etiology of Alzheimer's disease (AD), multifunctional agents may be beneficial for the treatment of this disease. A series of DL-3-n-butylphthalide-Edaravone hybrids were designed, synthesized and evaluated as novel dual inhibitors of amyloid-β aggregation and monoamine oxidases. Among them, co...

journal_title：Bioorganic & medicinal chemistry letters

authors： Qiang X,Li Y,Yang X,Luo L,Xu R,Zheng Y,Cao Z,Tan Z,Deng Y

更新日期：2017-02-15 00:00:00

abstract：:A series of diaryl ureas with an amide substitution at the 4-position was prepared and found to be potent and selective FLT3 inhibitors with good oral bioavailability and efficacy in a tumor xenograft model. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Patel HK,Grotzfeld RM,Lai AG,Mehta SA,Milanov ZV,Chao Q,Sprankle KG,Carter TA,Velasco AM,Fabian MA,James J,Treiber DK,Lockhart DJ,Zarrinkar PP,Bhagwat SS

更新日期：2009-09-01 00:00:00